|Systematic (IUPAC) name|
|Mol. mass||408.873 g/mol|
|(what is this?)|
Dapagliflozin (INN/USAN, trade name Forxiga) is a drug used to treat type 2 diabetes. It was developed by Bristol-Myers Squibb in partnership with AstraZeneca. Although dapagliflozin's method of action would operate on both types of diabetes and other conditions resulting in hyperglycemia, the current clinical trials specifically exclude participants with type 1 diabetes.
In July 2011 an US Food and Drug Administration (FDA) committee recommended against approval until more data was available. The Prescription Drug User Fee Act (PDUFA) date for dapagliflozin for the treatment of Type 2 diabetes was extended three months by the FDA to January 28, 2012.
In April 2012, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency issued a positive opinion on the drug. It is now marketed in a number of European countries including the UK and Germany.
Method of action
Dapagliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine. The efficacy of the this medication class has yet to be determined, but in initial clinical trials, dapagliflozin lowers HbA1c by 0.90 percentage points when added to metformin.
Since dapagliflozin leads to heavy glycosuria (sometimes up to about 70 grams per day) it can lead to rapid weight loss and tiredness. The glucose acts as an osmotic diuretic (this effect is the cause of polyuria in diabetes) which can lead to dehydration. The increased amount of glucose in the urine can also worsen the infections already associated with diabetes, particularly urinary tract infections and thrush (candidiasis). Dapagliflozin is also associated with hypotensive reactions.
- Statement on a nonproprietory name adopted by the USAN council
- Efficacy and Safety of Dapagliflozin, Added to Therapy of Patients With Type 2 Diabetes With Inadequate Glycemic Control on Insulin, ClinicalTrials.gov, April 2009
- Trial Details for Trial MB102-020, Bristol-Myers Squibb, May 2009
- "FDA panel advises against approval of dapagliflozin". 19 July 2011.
- Prous Science: Molecule of the Month November 2007
- UEndocrine: Internet Endocrinology Community
- Schubert-Zsilavecz, M, Wurglics, M, Neue Arzneimittel 2008/2009